• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

一些新型噻唑基-恶二唑啉的合成、亲脂性及抗菌活性评价

Synthesis, lipophilicity and antimicrobial activity evaluation of some new thiazolyl-oxadiazolines.

作者信息

Stoica Cristina Ioana, IonuȚ Ioana, Pîrnău Adrian, Pop Carmen, Rotar AncuȚa, Vlase Laurian, Oniga Smaranda, Oniga Ovidiu

机构信息

Therapeutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania.

出版信息

Clujul Med. 2015;88(4):521-9. doi: 10.15386/cjmed-473. Epub 2015 Nov 15.

DOI:10.15386/cjmed-473
PMID:26733751
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4689246/
Abstract

BACKGROUND AND AIMS

Synthesis of new potential antimicrobial agents and evaluation of their lipophilicity.

METHODS

Ten new thiazolyl-oxadiazoline derivatives were synthesized and their structures were validated by 1H-NMR and mass spectrometry. The lipophilicity of the compounds was evaluated using the principal component analysis (PCA) method. The necessary data for applying this method were obtained by reverse-phase thin-layer chromatography (RP-TLC). The antimicrobial activities were tested in vitro against four bacterial strains and one fungal strain.

RESULTS

The lipophilicity varied with the structure but could not be correlated with the antimicrobial activity, since this was modest.

CONCLUSIONS

We have synthesized ten new heterocyclic compounds. After their physical and chemical characterization, we determined their lipophilicity and screened their antimicrobial activity.

摘要

背景与目的

新型潜在抗菌剂的合成及其亲脂性评估。

方法

合成了十种新型噻唑基-恶二唑啉衍生物，并通过¹H-NMR和质谱对其结构进行了验证。使用主成分分析（PCA）方法评估了化合物的亲脂性。应用该方法所需的数据通过反相薄层色谱（RP-TLC）获得。对四种细菌菌株和一种真菌菌株进行了体外抗菌活性测试。

结果

亲脂性随结构变化，但由于抗菌活性适中，故无法与之建立相关性。

结论

我们合成了十种新型杂环化合物。在对其进行物理和化学表征后，测定了它们的亲脂性并筛选了抗菌活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/af6576973bc2/cm-88-521f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/9202f94a5163/cm-88-521f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/767bcd3a1c3a/cm-88-521f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/af6576973bc2/cm-88-521f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/9202f94a5163/cm-88-521f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/767bcd3a1c3a/cm-88-521f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e0ec/4689246/af6576973bc2/cm-88-521f3.jpg

相似文献

1
Synthesis, lipophilicity and antimicrobial activity evaluation of some new thiazolyl-oxadiazolines.一些新型噻唑基-恶二唑啉的合成、亲脂性及抗菌活性评价
Clujul Med. 2015;88(4):521-9. doi: 10.15386/cjmed-473. Epub 2015 Nov 15.
2
Lipophilicity evaluation of some thiazolyl-1,3,4-oxadiazole derivatives with antifungal activity.一些具有抗真菌活性的噻唑基-1,3,4-恶二唑衍生物的亲脂性评价
Biomed Chromatogr. 2018 Jul;32(7):e4221. doi: 10.1002/bmc.4221. Epub 2018 Apr 2.
3
Assessment of Lipophilicity Parameters of Antimicrobial and Immunosuppressive Compounds.评估抗菌和免疫抑制化合物的亲脂性参数。
Molecules. 2023 Mar 21;28(6):2820. doi: 10.3390/molecules28062820.
4
Synthesis of new thiazolyl-pyrazolyl-1,2,3-triazole derivatives as potential antimicrobial agents.合成新型噻唑基-吡唑基-1,2,3-三唑衍生物作为潜在的抗菌剂。
Eur J Med Chem. 2019 Oct 1;179:649-659. doi: 10.1016/j.ejmech.2019.06.074. Epub 2019 Jun 27.
5
Lipophilicity as a Central Component of Drug-Like Properties of Chalchones and Flavonoid Derivatives.疏水性作为查耳酮和类黄酮衍生物类药性质的核心组成部分。
Molecules. 2019 Apr 17;24(8):1505. doi: 10.3390/molecules24081505.
6
Design, synthesis and antimicrobial evaluation of pyrimidin-2-ol/thiol/amine analogues.嘧啶 -2-醇/硫醇/胺类似物的设计、合成及抗菌活性评价
Chem Cent J. 2017 Jun 9;11(1):52. doi: 10.1186/s13065-017-0284-2.
7
Study of the Relationships between the Structure, Lipophilicity and Biological Activity of Some Thiazolyl-carbonyl-thiosemicarbazides and Thiazolyl-azoles.某些噻唑基-羰基-硫代氨基脲和噻唑基-唑类化合物的结构、亲脂性与生物活性之间的关系研究
Molecules. 2015 Dec 11;20(12):22188-201. doi: 10.3390/molecules201219841.
8
Synthesis and antimicrobial activity of 4-phenyl/cyclohexyl-5-(1-phenoxyethyl)-3-[N-(2-thiazolyl)acetamido]thio-4H-1,2,4-triazole derivatives.4-苯基/环己基-5-(1-苯氧基乙基)-3-[N-(2-噻唑基)乙酰胺基]硫代-4H-1,2,4-三唑衍生物的合成与抗菌活性
Eur J Med Chem. 2005 Jun;40(6):607-13. doi: 10.1016/j.ejmech.2005.01.007. Epub 2005 Mar 2.
9
New hydrazide-hydrazones of isonicotinic acid: synthesis, lipophilicity and in vitro antimicrobial screening.新型异烟酸酰腙类化合物的合成、亲脂性及体外抗菌活性筛选。
Chem Biol Drug Des. 2018 Apr;91(4):915-923. doi: 10.1111/cbdd.13158. Epub 2018 Jan 5.
10
Reversed- and normal-phase liquid chromatography in quantitative structure retention-property relationships of newly synthesized seco-androstene derivatives.反相和正相液相色谱法在新合成的甾体衍生物的定量结构保留性质关系中的应用。
J Pharm Biomed Anal. 2014 Jan;88:636-42. doi: 10.1016/j.jpba.2013.10.011. Epub 2013 Oct 25.

本文引用的文献

1
Synthesis and biological evaluation of new oxadiazoline-substituted naphthalenyl acetates as anticancer agents.新型恶二唑啉取代萘基乙酸酯类抗癌剂的合成与生物学评价
Eur J Med Chem. 2014 Nov 24;87:805-13. doi: 10.1016/j.ejmech.2014.10.015. Epub 2014 Oct 13.
2
Multivariate regression modelling of antifungal activity of some benzoxazole and oxazolo[4,5-b]pyridine derivatives.某些苯并恶唑和恶唑并[4,5-b]吡啶衍生物抗真菌活性的多元回归建模
Acta Chim Slov. 2013;60(4):756-62.
3
Reversed-phase liquid chromatography with octadecylsilyl, immobilized artificial membrane and cholesterol columns in correlation studies with in silico biological descriptors of newly synthesized antiproliferative and analgesic active compounds.
反相液相色谱法与十八烷基硅烷、固定化人工膜和胆固醇柱相关联的研究与新合成的抗增殖和镇痛活性化合物的计算生物学描述符相关联。
J Chromatogr A. 2013 Nov 29;1318:92-101. doi: 10.1016/j.chroma.2013.09.060. Epub 2013 Sep 23.
4
Synthesis, characterization and molecular docking studies of some new 1,3,4-oxadiazolines bearing 6-methylpyridine moiety for antimicrobial property.合成、表征及一些新型含 6-甲基吡啶基 1,3,4-恶二唑啉类化合物的分子对接研究及其抗菌性能。
Eur J Med Chem. 2013 Oct;68:394-404. doi: 10.1016/j.ejmech.2013.07.019. Epub 2013 Aug 14.
5
Reversed-phase thin-layer chromatography technique for the comparison of the lipophilicity of selected non-steroidal anti-inflammatory drugs.反相薄层色谱技术用于比较几种非甾体抗炎药物的脂溶性。
J Pharm Biomed Anal. 2013 Nov;85:132-7. doi: 10.1016/j.jpba.2013.07.017. Epub 2013 Jul 25.
6
Lipophilicity--methods of determination and its role in medicinal chemistry.亲脂性——测定方法及其在药物化学中的作用。
Acta Pol Pharm. 2013 Jan-Feb;70(1):3-18.
7
Study of lipophilicity and membrane partition of 4-hydroxycoumarins by HPLC and PCA.用 HPLC 和 PCA 研究 4-羟基香豆素的亲脂性和膜分配。
J Pharm Biomed Anal. 2013 Mar 25;76:104-11. doi: 10.1016/j.jpba.2012.11.043. Epub 2012 Dec 14.
8
Quantification of Lipophilicity of 1,2,4-Triazoles Using Micellar Chromatography.使用胶束色谱法对1,2,4-三唑类化合物的亲脂性进行定量分析。
Chromatographia. 2012 May;75(9-10):449-456. doi: 10.1007/s10337-012-2227-3. Epub 2012 Apr 8.
9
Design, synthesis, biological evaluation and molecular modeling of 1,3,4-oxadiazoline analogs of combretastatin-A4 as novel antitubulin agents.1,3,4-噁二唑啉类似物的设计、合成、生物评价及分子模拟作为新型抗微管蛋白试剂的 combretastatin-A4。
Bioorg Med Chem. 2012 Jan 15;20(2):903-9. doi: 10.1016/j.bmc.2011.11.057. Epub 2011 Dec 3.
10
Synthesis and antimicrobial activity of some new thiazole, thiophene and pyrazole derivatives containing benzothiazole moiety.含苯并噻唑部分的噻唑、噻吩和吡唑衍生物的合成及抗菌活性。
Eur J Med Chem. 2010 Sep;45(9):3692-701. doi: 10.1016/j.ejmech.2010.05.018. Epub 2010 May 15.